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Published on: August 15, 2016
Enhancing the Drug Release and Physicochemical Properties of Rivaroxaban via Cyclodextrin Complexation: A
Cristina Solomon1, Valentina Anuța2, Iulian Sarbu3
1Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia St., 020956 Bucharest, Romania.
This study enhanced rivaroxaban solubility using cyclodextrin inclusion complexes and lyophilization. The resulting formulations showed improved stability and dissolution, comparable to commercial Xarelto.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Rivaroxaban exhibits poor aqueous solubility, limiting its bioavailability and therapeutic efficacy.
- Oral anticoagulants require improved formulation strategies for enhanced drug delivery.
- Cyclodextrins are widely used to improve the solubility of poorly soluble drugs.
Purpose of the Study:
- To enhance rivaroxaban solubility and dissolution characteristics.
- To formulate stable rivaroxaban inclusion complexes using cyclodextrin derivatives.
- To investigate the synergistic effect of cyclodextrin inclusion and lyophilization.
Main Methods:
- Formation of inclusion complexes using beta-cyclodextrin (β-CD), methyl-β-cyclodextrin (Me-β-CD), and hydroxypropyl-β-cyclodextrin (HP-β-CD).
- Lyophilization technique for complex preparation and stabilization.
- Physicochemical characterization using FTIR, SEM, XRD, and TGA.
Main Results:
- FTIR confirmed non-covalent interactions and encapsulation of rivaroxaban within cyclodextrins.
- SEM and XRD showed a transformation to a porous, amorphous matrix with reduced drug crystallinity.
- TGA indicated improved thermal stability of the inclusion complexes.
- Pharmacotechnical evaluation demonstrated suitable properties for direct compression.
Conclusions:
- Cyclodextrin inclusion complexes and lyophilization synergistically enhance rivaroxaban solubility and dissolution.
- The developed formulations exhibit improved characteristics compared to pure rivaroxaban.
- These strategies offer potential for developing effective rivaroxaban solid dosage forms.
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